Baragana, Beatriz published the artcileDiscovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy, Product Details of C11H13BrFNO, the main research area is quinoline carboxamide derivative preparation malaria translation elongation factor.
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen against the blood stage of Plasmodium falciparum (3D7) and displayed moderate potency but with suboptimal physicochem. properties and poor microsomal stability. The screening hit (1, EC50 = 120 nM) was optimized to lead mols. with low nanomolar in vitro potency. Improvement of the pharmacokinetic profile led to several compounds showing excellent oral efficacy in the P. berghei malaria mouse model with ED90 values below 1 mg/kg when dosed orally for 4 days. The favorable potency, selectivity, DMPK properties, and efficacy coupled with a novel mechanism of action, inhibition of translation elongation factor 2 (PfEF2), led to progression of 2 (DDD107498) to preclin. development.
Journal of Medicinal Chemistry published new progress about Antimalarials. 338454-98-1 belongs to class bromides-buliding-blocks, name is 4-(4-Bromo-2-fluorobenzyl)morpholine, and the molecular formula is C11H13BrFNO, Product Details of C11H13BrFNO.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary